Method for preparing effective monomer of total alkaloid extract of holarrhena antidysenterica and application thereof

A technology of total alkaloids and extracts, which is applied in the medical field of total alkaloids extracts of Antidiarrhea

Active Publication Date: 2011-08-17
LANZHOU UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But so far, there have been no reports on the prevention of Alzheimer's disease and the improvement of intelligence of the total alkaloid extract of Zhixie wood and its effective monomer components

Method used

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  • Method for preparing effective monomer of total alkaloid extract of holarrhena antidysenterica and application thereof
  • Method for preparing effective monomer of total alkaloid extract of holarrhena antidysenterica and application thereof
  • Method for preparing effective monomer of total alkaloid extract of holarrhena antidysenterica and application thereof

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preparation example Construction

[0013] The effective monomer preparation method and application of the total alkaloid extract of antidiarrheal wood, the steps of the method are:

[0014] (1) Zhixie wood is reflux extracted with 90% ethanol to obtain the ethanol extract;

[0015] (2) Dissolve the ethanol extract in water, then adjust the pH value to 1-2 with concentrated hydrochloric acid, and filter;

[0016] (3) The filtered filtrate is adjusted to a pH value of 9-11 with concentrated ammonia water or aqueous sodium hydroxide solution, and then extracted with an organic solvent to obtain the total alkaloid extract of the above-mentioned antidiarrheal wood.

[0017] (4) The total alkaloid extract is subjected to MCI-gel column chromatography, methanol aqueous solution gradient elution, and the steps of thin-layer chromatography detection to obtain effective monomer components of conessine and isoconessimine , conessimin, conarrhimin, conimin.

[0018] The use of the total alkaloid extract of the antidiarrh...

Embodiment 1

[0036] Example 1 The preparation of total alkaloid extract of antidiarrheal wood

[0037] Weigh 2.5 kg of antidiarrheal wood powder and place it in a round bottom flask, add 15 L of 90% ethanol for hot reflux extraction for 2 hours, and suction-filter to obtain the filtrate; then add 15 L of 90% ethanol for hot-reflux extraction for 1 hour, and then suction-filter to obtain the filtrate. The two filtrates were combined and concentrated to dryness, dissolved in 3 L of distilled water, adjusted to pH 1-2 with concentrated hydrochloric acid, left to stand for 15 hours and then suction filtered. The filtrate was adjusted to pH 9-11 with 2M aqueous sodium hydroxide solution or concentrated ammonia water. 3 L of chloroform was added each time for extraction, a total of 2 extractions, and the extracts were combined and concentrated to dryness to obtain 19 g of total alkaloids of C. chinensis.

Embodiment 2

[0038] Embodiment 2 Separation of effective monomer components

[0039] Get 19g of the total alkaloid extract of Diarrhea, dissolve it in methanol and use 200g MCI-gel (CHP 20P75-150μm) column chromatography, methanol aqueous solution (50%, 60%, 70%, 80%, 90% methanol) gradient Elution TLC detection combined the same components to obtain fractions A (3g), B (8g), C (4g). Fraction C was recrystallized with methanol to obtain compound 1 (3300mg); Fraction B was eluted with 200g silica gel column chromatography with chloroform-methanol solution gradient (40:1--5:1) (wherein the gradient elution solution contained 0.1% Ammonia) thin-layer chromatographic detection combined same components to obtain fraction B-1 (3g), B-2 (1.5g), B-3 (1g), B-4 (1g), fraction B-1 was washed with methanol Recrystallization obtains compound 5 (2800mg), fraction B-2 obtains compound 2 (1000mg) through methanol recrystallization, fraction B-3 uses 50g silica gel column chromatography chloroform-methano...

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Abstract

The invention discloses a method for preparing an effective monomer of a total alkaloid extract of holarrhena antidysenterica and application thereof. The method comprises the following steps of: (1) refluxing and extracting holarrhena antidysenterica by using 90 percent ethanol to obtain an ethanol extract; (2) dissolving the ethanol extract in water, regulating the pH value to be between 1 and 2 by using concentrated hydrochloric acid, and filtering; (3) regulating the pH value of filtrate obtained after the filtration to be between 9 and 11 by using stronger ammonia water or aqueous solution of sodium hydroxide, and extracting by using an organic solvent to obtain the total alkaloid extract of the holarrhena antidysenterica; and (4) performing MCI-gel column chromatography, methanol aqueous solution gradient elution, and thin-layer chromatography on the total alkaloid extract, wherein obtained effective monomer ingredients comprise conessine, isoconessimine, conessimin and conimin.The invention discloses application of the total alkaloid extract of the holarrhena antidysenterica in preparing medicaments for preventing and treating Alzheimer disease or medicaments for improvingintelligence, and application of the effective monomer ingredients of the total alkaloid extract of holarrhena antidysenterica in preparing the medicaments for preventing and treating Alzheimer disease or the medicaments for improving intelligence.

Description

technical field [0001] The invention relates to the medical technology related to the total alkaloid extract of antidiarrheal wood. Background technique [0002] Alzheimer's disease (Alzheimer's disease, referred to as senile dementia, referred to as AD) is a chronic progressive brain degenerative disease, clinically with cognitive decline as the core symptom. The incidence of AD is positively correlated with age, and it is the main type of senile dementia. In recent years, clinical studies at home and abroad have shown that the lack of acetylcholine in the brain of AD patients may be the cause of dementia, and acetylcholinesterase can hydrolyze acetylcholine in the brain, resulting in the lack of acetylcholine in the brain. Therefore, drugs that inhibit acetylcholinesterase can significantly increase the level of acetylcholine in the brain of AD patients, and play a role in preventing and treating senile dementia (Jin Youyu Pharmacology (Fifth Edition), 2001; 54-55). [0...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P25/00A61K36/24A61K31/58A61P25/28C07J71/00
Inventor 杨中铎段东柱李涛杨明俊任晋
Owner LANZHOU UNIVERSITY OF TECHNOLOGY
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